Metronidazol-akos

General characteristics. Structure:

Deystvuyubshchy вещесьво: 1 ml 1 фл. metronidazole of 5 mg 500 mg;

Excipients: disodium salt of ethylene diamine tetraacetic acid, water for and.

Description: solution for infusions of 0.5% transparent, with a greenish shade.

Pharmacological properties:

Antiprotozoan and antimicrobic drug, derivative 5 nitroimidazoles. The mechanism of action consists in biochemical recovery 5 nitrogroups intracellular transport proteins of anaerobic microorganisms and protozoa. The recovered 5 nitrogroup interacts with DNA of a cell of microorganisms, inhibiting synthesis of their nucleic acids that leads to death of bacteria.

Drug is active in the relation: Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp.; anaerobic bacteria: Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella spp. (Prevotella bivia, Prevotella buccae, Prevotella disiens), Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp. MPK for these strains makes 0.125-6.25 mkg/ml.

In combination with amoxicillin shows activity concerning Helicobacter pylori (amoxicillin suppresses development of resistance to metronidazole).

Aerobic microorganisms and facultative anaerobes, but in the presence of the mixed flora are steady against drug (aerobes and anaerobe bacterias) metronidazole works synergy with antibiotics, effective against aerobes.

Drug increases sensitivity of tumors to radiation, has disulfiramopodobny effect, stimulates reparative processes.

 

Pharmacokinetics. Absorption

Later in/in introductions in a dose of 500 mg within 20 min. Cmax in blood serum in 1 h makes 35.2 mkg/ml, in 4 h – 33.9 mkg/ml, in 8 h – 25.7 mkg/ml; Cmin at the subsequent introduction – 18 mkg/ml.

At in introduction of Cmax it is reached in 30-60 min., therapeutic concentration remains during 6-8 h.

At a normal bile production concentration of metronidazole in bile in/in introductions can exceed later considerably concentration in plasma.

Distribution

Linkng with proteins of plasma – 10-20%. Vd adults – 0.55 l/kg, at newborns have 0.54-0.81 l/kg.

Metronidazole has high penetration. Reaches bactericidal concentration in lungs, kidneys, a liver, a brain, skin, cerebrospinal fluid, bile, saliva, amniotic liquid, a cavity of abscesses, a vaginal secret, semen, breast milk. Gets through GEB, passes through a placental barrier.

Metabolism

It is metabolized (about 30-60%) by a hydroxylation, oxidation and a glyukuronirovaniye. The main metabolite – the 2nd oxymetronidazole – has antiprotozoan and antimicrobic effect.

Removal

20% - in not changed look are removed by kidneys (60-80%); through intestines 6-15% are removed. T1/2 is 8 h (6-12 h). Renal clearance – 10.2 ml/min.

Pharmacokinetics in special clinical cases

At alcoholic damage of a liver of T1/2 makes 18 h (10-29 h), at the newborns who were born at duration of gestation of 28-30 weeks – 75 h, at the term of 32-35 weeks – 35 h, at the term of 36-40 weeks – 25 h.

At patients with a renal failure after repeated introduction cumulation of metronidazole in blood serum can be observed.

Indications to use:

— protozoan infections (abenteric amebiasis / including liver abscess/, intestinal amebiasis, trichomoniasis, balanthidiasis, lambliasis (giardiasis), skin leushmaniosis, mecotic vaginitis, mecotic urethritis);

— the infections caused by Bacteroides spp., including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus (infections of bones and joints, TsNS infections / including meningitis, brain abscess/, bacterial endocarditis, pneumonia, empyema and abscess of lungs);

— the infections caused by Bacteroides spp. (including Bacteroides fragilis), Clostridium spp., Peptococcus spp., Peptostreptococcus spp. (infections of an abdominal cavity / peritonitis, liver abscess/, infections of bodies of a small pelvis / an endometritis, an endomyometritis, abscess of fallopian pipes and ovaries, infections of a vault of the vagina after surgical interventions/, infections of skin and soft tissues);

— the sepsis caused by Bacteroides spp. (including Bacteroides fragilis) and Clostridium spp.;

— the pseudomembranous colitis (connected using antibiotics);

— the gastritis or a peptic ulcer of a duodenum connected with Helicobacter pylori;

— alcoholism;

— as the radio sensibilizing means at radiation therapy (in cases when resistance of a tumor is caused by a hypoxia in tumor cells);

— prevention of postoperative infections (especially after operations on a colon, okolorektalny area, appendectomy, gynecologic interventions).

Route of administration and doses:

In kapelno adults and children 12 years drug are more senior appoint 0.5-1 g (duration of infusion of 30-40 min.) in an initial dose. Then each 8 h on 500 mg with a speed of 5 ml/min. At good tolerance after the first 2-3 infusions pass to jet introduction. A course of treatment – 7 days. If necessary in/in introduction continue during longer time. The maximum daily dose – 4 g. According to indications pass to the supporting intake in a dose 400 mg 3

To children aged up to 12 years appoint according to the same scheme in a single dose 7.5 mg/kg.

At it is purulent - septic diseases usually conduct 1 course of treatment.

In the preventive purposes to adults and children 12 years are more senior appoint kapelno 0.5-1 g on the eve of operation, in day of operation and next day – 1.5 g / (on 500 mg each 8 h). In 1-2 days pass to a maintenance therapy inside.

For patients with a chronic renal failure (at KK less than 30 ml/min.) the maximum daily dose makes 1 g.

As the radio sensibilizing means the drug is administered in/in kapelno, at the rate of 160 mg/kg or 4-6 g/m2 of a body surface for 0.5-1 h prior to radiation. Apply before each session of radiation within 1-2 weeks. During the remained radiotheraphy period metronidazole is not applied. The maximum single dose – 10 g, course – 60 g.

Apply drop administration of solutions of glucose, Haemodesum or isotonic solution of sodium of chloride to removal of intoxication caused by radiation.

At cancer of a neck of uterus and a body of the womb, a carcinoma cutaneum drug is used in the form of local applications (3 g dissolve in 10% dimethyl sulfoxide solution), moisten tampons which apply locally, for 1.5-2 h before radiation). At bad regression of a tumor of application carry out during all course of radiation therapy. At positive dynamics of clarification of a tumor from a necrosis – within the first 2 weeks.

Features of use:

It is necessary to consider that during use of drug ethanol reception since development of disulfiramopodobny reaction is possible is contraindicated (spastic abdominal pains, nausea, vomiting, a headache, sudden rush of blood to the person).

At long therapy it is necessary to control a blood pattern.

At a leukopenia the possibility of continuation of treatment depends on risk of development of infectious process.

At development of neurologic symptoms it is necessary to stop drug use.

At treatment of a mecotic vaginitis at women and a mecotic urethritis at men it is necessary to abstain from sex life. Simultaneous treatment of sexual partners is obligatory. During periods it is necessary to continue treatment. After the end of treatment of trichomoniasis it is necessary to conduct control researches during 3 next cycles before and after periods.

After the end of treatment of a lambliasis (if symptoms remain) in 3-4 weeks it is necessary to carry out 3 analyses a bucketed calla in several days (some successfully treated patients have a lactose intolerance caused by an invasion, can remain within several weeks or months, reminding lambliasis symptoms).

Drug can immobilize treponemas and lead to the false positive test of Nelson.

It is not recommended to combine with not depolarizing muscle relaxants (for example, a vekuroniya bromide).

Use in pediatrics

18 years are not recommended to use drug in a combination with amoxicillin at patients more young.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, intestinal colic, a lock, metal smack in a mouth, dryness in a mouth, a glossitis, stomatitis, pancreatitis.

From a nervous system: dizziness, incoordination of movements, ataxy, confusion of consciousness, irritability, depression, hypererethism, weakness, sleeplessness, headache, spasms, hallucinations, peripheral neuropathy.

From an urinary system: a dysuria, cystitis, a polyuria, an urine incontience, coloring of urine in red-brown color.

Allergic reactions: skin rash, small tortoiseshell, dermahemia, nose congestion, fever, arthralgia.

Local reactions: at in introduction – thrombophlebitis (pain, reddening, puffiness).

Others: candidiasis, a neutropenia, a leukopenia, flattening of a tooth of T on an ECG.

Interaction with other medicines:

At simultaneous use of metronidazole with indirect anticoagulants increase in time of formation of a prothrombin is noted.

At simultaneous use of Metronidazola-AKOS with drugs of salts of lithium increase in concentration of lithium in a blood plasma and development of symptoms of intoxication is possible.

At simultaneous use with Cimetidinum the metronidazole metabolism inhibition is noted that can lead to increase in concentration of metronidazole in a blood plasma and to increase in risk of development of side reactions.

At simultaneous use with metronidazole of the drugs stimulating enzymes of a microsomal oxidation in a liver (Phenytoinum, phenobarbital) metronidazole removal therefore its concentration in a blood plasma decreases can accelerate.

Streptocides strengthen antimicrobic effect of metronidazole.

At simultaneous use with ethanol development of disulfiramopodobny reactions is noted.

Pharmaceutical interaction

Metronidazole for in/in introductions is not recommended to be mixed with other medicines.

Contraindications:

— a leukopenia (including in the anamnesis);

— organic lesions of TsNS;

— epilepsy;

— a liver failure (at use of drug in high doses);

— pregnancy (I trimester);

— lactation (breastfeeding);

— hypersensitivity to drug.

 

Use of drug METRONIDAZOL-AKOS at pregnancy and feeding by a breast
With care it is necessary to appoint drug in II and III trimesters of pregnancy.

Drug is contraindicated to use in the I trimester of pregnancy and during breastfeeding.

 

Use at abnormal liver functions
It is contraindicated at a liver failure (at use of drug in high doses);

 

Use at renal failures
For patients with a chronic renal failure (at KK less than 30 ml/min.) the maximum daily dose makes 1 g.

 

Use for children
In kapelno children 12 years drug are more senior appoint 0.5-1 g (duration of infusion of 30-40 min.) in an initial dose. Then each 8 h on 500 mg with a speed of 5 ml/min. At good tolerance after the first 2-3 infusions pass to jet introduction. A course of treatment – 7 days. If necessary in/in introduction continue during longer time. The maximum daily dose – 4 g. According to indications pass to the supporting intake in a dose 400 mg 3

To children aged up to 12 years appoint according to the same scheme in a single dose 7.5 mg/kg.

In the preventive purposes to children 12 years are more senior appoint kapelno 0.5-1 g on the eve of operation, in day of operation and next day – 1.5 g / (on 500 mg each 8 h). In 1-2 days pass to a maintenance therapy inside.

Overdose:

Data on overdose of drug are absent.

Treatment: metronidazole and the main metabolites quickly are removed at a hemodialysis (T1/2 is reduced to 2.6 h). At peritoneal dialysis it is removed in insignificant quantities.

Storage conditions:

List B. Drug should be stored in protected from light, the place, unavailable to children, at a temperature from 15 °C to 25 °C. A period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

100 ml - bottles of dark glass (1) - a pack cardboard.